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Merck
CN

573128

STAT3 Inhibitor XIII, C188-9

The Stat3 Inhibitor XIII, C188-9 controls the biological activity of Stat3. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

别名:

STAT3 Inhibitor XIII, C188-9, N-(1ʹ,2-Dihydroxy-1,2ʹ-binaphthalen-4ʹ-yl)-4-methoxybenzenesulfonamide, F1113-0789

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关于此项目

经验公式(希尔记法):
C27H21NO5S
化学文摘社编号:
分子量:
471.52
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Form:
powder
Storage condition:
OK to freeze, protect from light
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Quality Segment

assay

≥98% (HPLC)

form

powder

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

color

off-white to pale beige

solubility

DMSO: 100 mg/mL

shipped in

ambient

storage temp.

2-8°C

SMILES string

OC1=C(C2=C(O)C=CC3=C2C=CC=C3)C=C(NS(C(C=C4)=CC=C4OC)(=O)=O)C5=C1C=CC=C5

InChI key

QDCJDYWGYVPBDO-UHFFFAOYSA-N

General description

A cell-permeable binaphthol-sulfonamide that competes against pY proteins for Stat3 SH2 domain binding. Shown to inhibit G-CSF-induced (100 ng/ml for 15 min following 1 h drug pretreatment) Stat3 tyr705 phosphorylation in 6 human AML cell lines (IC50 from 4.1 to 8.3 µM) and 4 primary pediatric AML cultures (IC50 from 8 to 18 µM). Long-term treatments (24 h for lines and 48 h for primary cultures) result in apoptosis induction (Annexin V-PE staining) in 7 AML lines (EC50 from 8.4 to 43.6 µM) and CD34+ populations from 5 primary pediatric AML samples (EC50 from 0.8 to25 µM). Selectivity studies using Kasumi-1 cells reveals concomitant inhibitions of G-CSF-stimulated TIE2, MATK, JAK1, and HGFR phosphorylation (by 90%, 50%, 40%, and 40%, respectively; 10 µM C188-9), but not 15 other phosphoproteins (≤30% inhibition), including pERK1/2 and pAKT.

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Redell, M.S., et al. 2011. Blood112, 355.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Toxic (F)


存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable



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